Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives. 2. 7-Acyl amide analogs

1983 ◽  
Vol 26 (3) ◽  
pp. 403-411 ◽  
Author(s):  
C. John Blankley ◽  
Lawrence R. Bennett ◽  
Robert W. Fleming ◽  
Ronald D. Smith ◽  
Deirdre K. Tessman ◽  
...  
Keyword(s):  
Antihypertensive Activity ◽  
Acyl Amide

ChemInform Abstract: ANTIHYPERTENSIVE ACTIVITY OF 6-ARYLPYRIDO(2,3-D)PYRIMIDIN-7-AMINE DERIVATIVES. 2. 7-ACYL AMIDE ANALOGS

1983 ◽  
Vol 14 (34) ◽  
Author(s):  
C. J. BLANKLEY ◽  
L. R. BENNETT ◽  
R. W. FLEMING ◽  
R. D. SMITH ◽  
D. K. TESSMAN ◽  
...  
Keyword(s):  
Antihypertensive Activity ◽  
Acyl Amide

Characterization and functional properties of new everbearing strawberry (Fragaria x ananasa Duch.) cultivar, ‘Summertiara’ berries

2014 ◽  
Vol 4 (1) ◽  
pp. 1 ◽  
Author(s):  
Takeshi Nagai ◽  
Misuzu Tamai ◽  
Masato Sato ◽  
Yasuhiro Tanoue ◽  
Norihisa Kai ◽  
...  
Keyword(s):  
Vitamin C ◽  
Sensory Evaluation ◽  
Functional Properties ◽  
Active Oxygen Species ◽  
Active Oxygen ◽  
Antihypertensive Activity ◽  
Oxygen Species ◽  
Total Anthocyanins ◽  
Strawberry Cultivar ◽  
The Stability

Background: In recent years, a new everbearing strawberry cultivar, ‘Summertiara’ was cultivated to supply the strawberries in pre-harvest season from July to October in Japan. For highly research and development of processing of this cultivar, ‘Summertiara’ berries, the objective of this study was to characterize these berries, with relation to chemical parameters, total phenols, total flavonoids, total vitamin C, and total anthocyanins, and was to investigate the solubility and the stability of anthocyanins from the berries. Moreover, the functional properties such as antioxidative activity, active oxygen species scavenging activity, and antihypertensive activity were also evaluated.Methods: Chemical analysis, colour measurement, and sensory evaluation of new everbearing strawberry cultivar, ‘Summertiara’ berries were performed. Next, the solubility of anthocyanins from the berries and stability of these against pH, temperature, and an incandescent lighting were investigated. Moreover, functional properties of the extracts prepared from berries were elucidated using 5 different methods.Results: The contents of water, proteins, lipids, carbohydrates, and ash were the same as those of other cultivar berries. The sugar-acid ratio in the berries was low; these were acidulous. By sensory evaluation, the main factors were vivid red colour, aroma, and acidity. The berries were rich in phenols, flavonoids, vitamin C, and anthocyanins. The anthocyanins of the berries became unstable by heat treatment and light exposures such as visible rays. On the other hand, the extracts prepared from the berries showed the functionalities such as antioxidant activity, active oxygen species scavenging activities, and antihypertensive activity.  Conclusions: The strawberry cultivar, ‘Summertiara’ berries were the most suitable for processing ingredient of strawberry-derived products with superior health promoting functionalities.Keywords: Summertiara, everbearing strawberry cultivar, characterization, sensory evaluation, color and storage, functional property

PDO Rotonda’s Red Eggplant Extract: In vitro Determination of Biological Properties and Minerals Bioaccessibility

2020 ◽  
Vol 16 (1) ◽  
pp. 65-74
Author(s):  
Ortensia Ilaria Parisi ◽  
Mariarosa Ruffo ◽  
Fabio Amone ◽  
Rocco Malivindi ◽  
Domenico Gorgoglione ◽  
...  
Keyword(s):  
Control Sample ◽  
Specific Area ◽  
Biological Properties ◽  
Ammonium Molybdate ◽  
Antihypertensive Activity ◽  
Protected Designation Of Origin ◽  
The Family ◽  
Oil Red O Staining

Background: The Rotonda’s Red Eggplant belongs to the family of Solanum aethiopicum and it is cultivated in a specific area of Potenza (Basilicata, South of Italy) including villages of Rotonda, Viggianello, Castelluccio Superiore and Castelluccio Inferiore. The Red Eggplant cultivated in this area has gained the PDO, “Protected Designation of Origin”. Objective: The aim of this research was to evaluate the use of PDO Rotonda’s Red Eggplant extract as a possible nutraceutical supplement. The antioxidant, antihypertensive, hypoglycemic, and hypolipidemic properties were in vitro evaluated. Methods: The antioxidant activity was investigated by evaluating the scavenging properties against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-Azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals and by performing the Ammonium Molybdate and Folin-Ciocalteu assay. The hypoglycemic and antihypertensive activity was studied by evaluating the α-Amylase, α-Glucosidase and Angiotensin Converting Enzyme, respectively, inhibiting activity. In order to evaluate the hypolipidemic activity, the pancreatic lipase inhibiting property was determined and Oil Red O staining assay was performed. Finally, to evaluate the possible use of this extract as a minerals supplement, Selenium, Potassium and Chrome bioaccessibility was studied. Results: The obtained results underline the good antioxidant, hypoglycemic, antihypertensive and hypolipidemic in vitro properties of the PDO Rotonda’s Red Eggplant extract. Moreover, the obtained data show a higher minerals bioaccessibility and this higher value could be ascribable to the natural phytocomplex of PDO Rotonda’s Red Eggplant, which increases the minerals bioaccessibility if compare it with a control sample. Conclusion: The obtained results show that PDO Rotonda’s Red Eggplant extract, might be used as a possible nutraceutical supplement, along with traditional therapies, both for its biological properties and for its minerals bioaccessibility value.

Hetero-Tricyclic Lead Scaffold as Novel PDE5A Inhibitor for Antihypertensive Activity: In Silico Docking Studies

2019 ◽  
Vol 15 (4) ◽  
pp. 318-333
Author(s):  
Dipak P. Mali ◽  
Neela M. Bhatia
Keyword(s):  
In Silico ◽  
Docking Study ◽  
Docking Studies ◽  
Antihypertensive Activity ◽  
In Silico Docking ◽  
Π Stacking ◽  
Π Stacking Interaction ◽  
Nitrogen Heteroatom ◽  
Inhibitory Potential ◽  
Vlife Mds

Objective:To screen the phytochemicals for phosphodiesterase 5A (PDE5A) inhibitory potential and identify lead scaffolds of antihypertensive phytochemicals using in silico docking studies.Methods:In this perspective, reported 269 antihypertensive phytochemicals were selected. Sildenafil, a PDE5A inhibitor was used as the standard. In silico docking study was carried out to screen and identify the inhibiting potential of the selected phytochemicals against PDE5A enzyme using vLife MDS 4.4 software.Results:Based on docking score, π-stacking, H-bond and ionic interactions, 237 out of 269 molecules were selected which have shown one or more interactions. Protein residue Gln817A was involved in H-boding whereas Val782A, Phe820A and Leu804A were involved in π-stacking interaction with ligand. The selected 237 phytochemicals were structurally diverse, therefore 82 out of 237 molecules with one or more tricycles were filtered out for further analysis. Amongst tricyclic molecules, 14 molecules containing nitrogen heteroatom were selected for lead scaffold identification which finally resulted in three different basic chemical backbones like pyridoindole, tetrahydro-pyridonaphthyridine and dihydro-pyridoquinazoline as lead scaffolds.Conclusion:In silico docking studies revealed that nitrogen-containing tetrahydro-pyridonaphthyridine and dihydro-pyridoquinazoline tricyclic lead scaffolds have emerged as novel PDE5A inhibitors for antihypertensive activity. The identified lead scaffolds may provide antihypertensive lead molecules after its optimization.

Ruta montana evokes antihypertensive activity through increase of prosta-glandins release in L-NAME-induced hypertensive rats

2020 ◽  
Vol 20 ◽  
Author(s):  
El-Ouady Fadwa ◽  
Mohamed Eddouks
Keyword(s):  
Blood Pressure ◽  
Heart Rate ◽  
Aqueous Extract ◽  
Antihypertensive Effect ◽  
Antihypertensive Activity ◽  
Computer Assisted ◽  
Hypertensive Rats ◽  
Vasorelaxant Effect ◽  
Vasorelaxant Activity ◽  
Ruta Montana

Aims: The aim of the study was to investigate experimentally the antihypertensive effect of Ruta Montana. Background: Ruta montana L. is traditionally used in Moroccan herbal medicine to treat hypertension. This study aimed to evaluate experimentally the hypotensive and vasoactive properties of this plant. Objective: The objective of the study was to evaluate the effect of the aqueous extract of Ruta Montana on blood pressure parameters in LNAME-induced hypertensive rats and to determine the vasorelaxant activity of this aqueous extract. Methods: The antihypertensive effect of the aqueous extract obtained from Ruta montana aerial parts (RMAPAE) (200 mg/kg) was evaluated in normal and anesthetized hypertensive rats. Blood pressure parameters (systolic blood pressure (SBP), mean blood pressure (MBP) and diastolic blood pressure (DBP)) and heart rate were measured using a tail-cuff and a computer-assisted monitoring device. The acute and chronic effect of RMAPAE was recorded during 6 hours for the acute experiment and during 7 days for the sub-chronic test. In the other set, the vasorelaxant effect of RMAPAE on the contractile response was undertaken in isolated thoracic aorta. Results: The results indicated that RMAPAE extract significantly decreased SBP, MBP, DBP and heart rate in L-NAMEinduced hypertensive rats. Furthermore, RMAPAE was demonstrated to induce a dose dependent relaxation in the aorta precontracted with Epinephrine or KCl. More interestingly, this vasorelaxant activity of RMAPAE seems to be probably mediated through the prostaglandins pathway. Conclusion: The present study illustrates the beneficial action of Ruta montana on hypertension and supports then its use as an antihypertensive agent.

Cardiovascular Effects of Micromeria graeca (L.) Benth. ex Rchb in Normotensive and Hypertensive Rats

2020 ◽  
Vol 20 (8) ◽  
pp. 1253-1261
Author(s):  
Mourad Akdad ◽  
Mohamed Eddouks
Keyword(s):  
Blood Pressure ◽  
Cardiovascular System ◽  
Arterial Blood Pressure ◽  
Antihypertensive Activity ◽  
Computer Assisted ◽  
Hypertensive Rats ◽  
Vasorelaxant Effect ◽  
Arterial Blood

Aims: The present study was performed in order to analyze the antihypertensive activity of Micromeria graeca (L.) Benth. ex Rchb. Background: Micromeria graeca (L.) Benth. ex Rchb is an aromatic and medicinal plant belonging to the Lamiaceae family. This herb is used to treat various pathologies such as cardiovascular disorders. Meanwhile, its pharmacological effects on the cardiovascular system have not been studied. Objective: The present study aimed to evaluate the effect of aqueous extract of aerial parts of Micromeria graeca (AEMG) on the cardiovascular system in normotensive and hypertensive rats. Methods: In this study, the cardiovascular effect of AEMG was evaluated using in vivo and in vitro investigations. In order to assess the acute effect of AEMG on the cardiovascular system, anesthetized L-NAME-hypertensive and normotensive rats received AEMG (100 mg/kg) orally and arterial blood pressure parameters were monitored during six hours. In the sub-chronic study, rats were orally treated for one week, followed by blood pressure assessment during one week of treatment. Blood pressure was measured using a tail-cuff and a computer-assisted monitoring device. In the second experiment, isolated rat aortic ring pre-contracted with Epinephrine (EP) or KCl was used to assess the vasorelaxant effect of AEMG. Results: Oral administration of AEMG (100 mg/kg) provoked a decrease of arterial blood pressure parameters in hypertensive rats. In addition, AEMG induced a vasorelaxant effect in thoracic aortic rings pre-contracted with EP (10 μM) or KCl (80 mM). This effect was attenuated in the presence of propranolol and methylene blue. While in the presence of glibenclamide, L-NAME, nifedipine or Indomethacin, the vasorelaxant effect was not affected. Conclusion: This study showed that Micromeria graeca possesses a potent antihypertensive effect and relaxes the vascular smooth muscle through β-adrenergic and cGMP pathways.

Vasorelaxant and Antihypertensive Effects of Mentha pulegium L. in Rats: An in vitro and in vivo Approach

2020 ◽  
Vol 20 ◽  
Author(s):  
Mohammed Ajebli ◽  
Mohamed Eddouks
Keyword(s):  
Blood Pressure ◽  
Acute Experiment ◽  
Antihypertensive Activity ◽  
Mentha Pulegium ◽  
In Vitro Experiment ◽  
Arterial Blood ◽  
Dose Dependent ◽  
Ca2 Channels

Aims and objective: The aim of the study was to investigate the effect of aqueous aerial part extract of Mentha pulegium L. (Pennyrile) (MPAE) on arterial pressure parameters in rats. Background: Mentha pulegium is a medicinal plant used to treat hypertension in Morocco. Material and methods: In the current study, MPAE was prepared and its antihypertensive activity was pharmacologically investigated. L-NAME-hypertensive and normotensive rats have received orally MPAE (180 and 300 mg/kg) during six hours for the acute experiment and during seven days for the sub-chronic treatment. Thereafter, systolic, diastolic, mean arterial blood pressure and heart rate were evaluated. While, in the in vitro experiment, isolated denuded and intact thoracic aortic rings were suspended in a tissue bath system and the tension changes were recorded. Results: A fall in blood pressure was observed in L-NAME-induced hypertensive treated with MPAE. The extract also produced a dose-dependent relaxation of aorta pre-contracted with NE and KCl. The study showed that the vasorelaxant ability of MPAE seems to be exerted through the blockage of extracellular Ca2+ entry. Conclusion: The results demonstrate that the extract of pennyrile exhibits antihypertensive activity. In addition, the effect may be, at least in part, due to dilation of blood vessels via blockage of Ca2+ channels.

Synthesis and ocular antihypertensive activity of new imidazolidine derivatives containing a .beta.-blocking side chain

1991 ◽  
Vol 34 (11) ◽  
pp. 3197-3204 ◽  
Author(s):  
D. Huber ◽  
J. D. Ehrhardt ◽  
N. Decker ◽  
J. Himber ◽  
G. Andermann ◽  
...  
Keyword(s):  
Side Chain ◽  
Antihypertensive Activity ◽  
Beta Blocking

scholarly journals ACE Inhibitory and Antihypertensive Activities of Wine Lees and Relationship among Bioactivity and Phenolic Profile

Nutrients ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 679
Author(s):  
Raúl López-Fernández-Sobrino ◽  
Jorge R. Soliz-Rueda ◽  
Maria Margalef ◽  
Anna Arola-Arnal ◽  
Manuel Suárez ◽  
...  
Keyword(s):  
Hypotensive Effect ◽  
Wine Industry ◽  
Antihypertensive Activity ◽  
Spontaneously Hypertensive ◽  
Lowering Effect ◽  
Before And After ◽  
Phenolic Profiles ◽  
Wistar Kyoto ◽  
Grape Varieties ◽  
The Relationship

Wine lees (WL) are by-products generated in the winemaking process. The aim of this study was to investigate the angiotensin-converting enzyme inhibitory (ACEi) activity, and the blood pressure (BP) lowering effect of WL from individual grape varieties. The relationship among their activities and phenolic profiles was also studied. Three WL, from Cabernet, Mazuela, and Garnacha grape varieties, were firstly selected based on their ACEi properties. Their phenolic profiles were fully characterized by UHPLC-ESI-Q-TOF-MS. Then, their potential antihypertensive effects were evaluated in spontaneously hypertensive rats (SHR). BP was recorded before and after their oral administrations (2, 4, 6, 8, 24, and 48 h) at a dose of 5 mL/kg bw. Cabernet WL (CWL) exhibited a potent antihypertensive activity, similar to that obtained with the drug Captopril. This BP-lowering effect was related to the high amount of anthocyanins and flavanols present in these lees. In addition, a potential hypotensive effect of CWL was discarded in normotensive Wistar–Kyoto rats. Finally, the ACEi and antihypertensive activities of CWL coming from a different harvest were confirmed. Our results suggest the potential of CWL for controlling arterial BP, opening the door to commercial use within the wine industry.

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